α-NETA
Catalog No.: GC45213Purity:>98.00%
α-NETA is a non-competitive inhibitor of choline acetyltransferase (ChAT; IC50=9μM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 115066-04-1
10mM (in 1mL DMSO)In Stock
$62.00
1
5mgIn Stock
$35.00
1
10mgIn Stock
$56.00
1
50mgIn Stock
$168.00
1
100mgIn Stock
$280.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $62.00 | In Stock | 1 | |
| 5mg | $35.00 | In Stock | 1 | |
| 10mg | $56.00 | In Stock | 1 | |
| 50mg | $168.00 | In Stock | 1 | |
| 100mg | $280.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Citations
2 publicationsPublications from researchers using this productDescription
α-NETA is a non-competitive inhibitor of choline acetyltransferase (ChAT; IC50=9μM). α-NETA inhibits ALDH1A1 (IC50=0.04μM) and antagonizes the activity of chemokine-like receptor 1 (CMKLR1), cholinesterase (ChE; IC50=84μM), and acetylcholinesterase (AChE; IC50=300μM). α-NETA can be used in research related to cancer and diabetic nephropathy[1-4].
In vitro, α-NETA (5μM) pretreated human gastric cancer AGS cells for 16-24 hours. α-NETA inhibited Chemerin-induced cell migration and invasion and suppressed cell morphological transformation[5]. α-NETA (3μM) treated chemerin-overexpressing human trophoblast cells (HTR8/SVneo) for 24-48 hours. α-NETA induced cell membrane rupture, cytoplasmic leakage, and activated the GSDMD/caspase-4-mediated pyroptosis pathway by increasing the expression of caspase-4 and GSDMD and the secretion of IL-18[6].
In vivo, α-NETA (30mg/kg; once daily) was administered by gavage to high-fat diet-induced obese C57BL/6 mice for 4 weeks. α-NETA reduced body weight in the mice[7]. α-NETA (10mg/kg; three times per week) was administered via intraperitoneal injection to nude mice bearing UOK101 cell xenograft tumors and SCID mice bearing human ccRCC PDX (UTSW-XP296) models (subcutaneous and orthotopic implantation) for 70 days. α-NETA significantly inhibited tumor growth and reduced lipid deposition within the tumors, while no significant changes in animal health status were observed[8].
References:
[1] Sastry BV, Jaiswal N, Janson V, et al. Relationships between chemical structure and inhibition of choline acetyltransferase by 2-(alpha-naphthoyl)ethyltrimethylammonium and related compounds. Pharmacol Res Commun. 1988 Sep;20(9):751-71.
[2] Graham KL, Zhang JV, Lewén S, et al. A novel CMKLR1 small molecule antagonist suppresses CNS autoimmune inflammatory disease. PLoS One. 2014 Dec 1;9(12):e112925.
[3] Qiao L, Wu X, Zhang J, et al. α-NETA induces pyroptosis of epithelial ovarian cancer cells through the GSDMD/caspase-4 pathway. FASEB J. 2019 Nov;33(11):12760-12767.
[4] Aleksandrov AA, Polyakova NV, Vinogradova EP, et al. The TAAR5 agonist α-NETA causes dyskinesia in mice. Neurosci Lett. 2019 Jun 21;704:208-211.
[5] Kumar JD, Aolymat I, Tiszlavicz L, et al. Chemerin acts via CMKLR1 and GPR1 to stimulate migration and invasion of gastric cancer cells: putative role of decreased TIMP-1 and TIMP-2. Oncotarget. 2019 Jan 4;10(2):98-112.
[6] Tan L, Chen Z, Sun F, et al. Placental trophoblast-specific overexpression of chemerin induces preeclampsia-like symptoms. Clin Sci (Lond). 2022 Feb 25;136(4):257-272.
[7] Zheng C, Zheng Y, Chen X, et al. α-NETA down-regulates CMKLR1 mRNA expression in ileum and prevents body weight gains collaborating with ERK inhibitor PD98059 in turn to alleviate hepatic steatosis in HFD-induced obese mice but no impact on ileal mucosal integrity and steatohepatitis progression. BMC Endocr Disord. 2023 Jan 10;23(1):9.
[8] Wang D, Mahmud I, Thakur VS, et al. GPR1 and CMKLR1 Control Lipid Metabolism to Support the Development of Clear Cell Renal Cell Carcinoma. Cancer Res. 2024 Jul 2;84(13):2141-2154.
Protocol
| Cell experiment [1]: | |
Cell lines | HTR8/SVneo cells (immortalized human trophoblast cells) |
Preparation Method | HTR8/SVneo cells were maintained in DMEM/F12 medium supplemented with 10% fetal bovine serum (FBS) at 37°C with 5% CO₂. Cells were infected with LV-hChemerin-GFP lentivirus to overexpress chemerin, selected with puromycin, and subsequently exposed to either 1% DMSO (vehicle control) or 3μM α-NETA dissolved in DMSO. |
Reaction Conditions | 3μM; 24-48h |
Applications | α-NETA prevented the inhibitory effects of chemerin overexpression on cell migration, invasion, and tube formation in co-culture with human umbilical vein endothelial cells (HUVECs). |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice (male, 8-10 weeks old) |
Preparation Method | Mice were fed a high-fat diet (HFD, 40 kcal% fat, 2% fructose) for 12 weeks to induce obesity. Then, mice in the α-NETA group received daily treatments of α-NETA (30mg/kg) via gavage for 4 weeks. Mice in the α-NETA+PD group received daily treatment of α-NETA plus PD98059 (0.3mg/kg via tail vein injection). At the end of intervention, mice were sacrificed for analysis of body weight, liver histology, ileal CMKLR1 mRNA, and serum parameters. |
Dosage form | 30mg/kg; daily gavage; for 4 weeks |
Applications | α-NETA reduced body weight gain in HFD-induced obese mice. Combined with PD98059, α-NETA further reduced body weight and alleviated hepatic steatosis. α-NETA down-regulated CMKLR1 mRNA expression in ileum. No impact on ileal ZO-1 or pERK protein expression, and no significant changes in serum endotoxin levels. |
References: | |
Product Documents
Purity:>98.00%Appearance:A solid
Chemical Properties
CAS No.
115066-04-1
SMILES
O=C(CC[N+](C)(C)C)C1=CC2=CC=CC=C2C=C1.[I-]
Molecular Formula
C16H20NO•I
Molecular Weight
369.2
Solubility
DMSO: 3mg/ml,Methanol: Soluble
Storage
Store at -20°C, protect from light, stored under nitrogen
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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